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Updated: May 8, 2026

Evaluating the Effectiveness of Cancer Drug Sensitization In Vitro and In Vivo
Published on: February 6, 2015
Pharmacogenetics/genomics of membrane transporters in cancer chemotherapy
1Department of Pharmaceutical Sciences, College of Pharmacy, Western University of Health Sciences, Pomona, CA 91766, USA. yhuang@westernu.edu
Abstract:
Inter-individual variability in drug response and the emergence of adverse drug reactions are main causes of treatment failure in cancer therapy. Recently, membrane transporters have been recognized as an important determinant of drug disposition, thereby affecting chemosensitivity and -resistance. Genetic factors contribute to inter-individual variability in drug transport and targeting. Therefore, pharmacogenetic studies of membrane transporters can lead to new approaches for optimizing cancer therapy. This review discusses genetic variations in efflux transporters of the ATP-binding cassette (ABC) family such as ABCB1 (MDR1, P-glycoprotein), ABCC1 (MRP1), ABCC2 (MRP2) and ABCG2 (BCRP), and uptake transporters of the solute carrier (SLC) family such as SLC19A1 (RFC1) and SLCO1B1 (SLC21A6), and their relevance to cancer chemotherapy. Furthermore, a pharmacogenomic approach is outlined, which using correlations between the growth inhibitory potency of anticancer drugs and transporter gene expression in multiple human cancer cell lines, has shown promise for determining the relevant transporters for any given drugs and predicting anticancer drug response.
Insights
Genetic variations in drug transporters significantly impact cancer treatment outcomes. Understanding these genetic factors offers new strategies for personalized cancer therapy and predicting drug response.
Area of Science:
- Pharmacogenomics
- Molecular Biology
- Cancer Therapy
Background:
- Inter-individual variability in drug response and adverse drug reactions contribute to cancer treatment failure.
- Membrane transporters play a crucial role in drug disposition, influencing chemosensitivity and resistance.
- Genetic factors are key determinants of this variability in drug transport and targeting.
Purpose of the Study:
- To review genetic variations in key efflux (ABC family) and uptake (SLC family) transporters.
- To discuss the relevance of these genetic variations in cancer chemotherapy.
- To outline a pharmacogenomic approach for predicting anticancer drug response.
Main Methods:
- Review of literature on genetic variations in ATP-binding cassette (ABC) and solute carrier (SLC) transporters.
- Analysis of correlations between anticancer drug potency and transporter gene expression in cancer cell lines.
Main Results:
- Genetic variations in transporters like ABCB1, ABCC1, ABCC2, ABCG2, SLC19A1, and SLCO1B1 are relevant to cancer chemotherapy.
- A pharmacogenomic approach shows promise in identifying relevant transporters and predicting drug response.
Conclusions:
- Pharmacogenetic studies of membrane transporters are vital for optimizing cancer therapy.
- Understanding transporter genetics can lead to more effective and personalized cancer treatments.
- A pharmacogenomic approach aids in predicting patient response to anticancer drugs.
Related Concept Videos
Pharmacogenetics and Pharmacogenomics: Overview
Pharmacogenetic Phenotypes: Alterations in Pharmacokinetics, Drug Targets and Biologic Milieu
Pharmacogenetics of Drug Metabolism: Overview
Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase
Pharmacogenomics: Identification of New Drug Targets

